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JP2011037841A5
JP2011037841A5 JP2010161144A JP2010161144A JP2011037841A5 JP 2011037841 A5 JP2011037841 A5 JP 2011037841A5 JP 2010161144 A JP2010161144 A JP 2010161144A JP 2010161144 A JP2010161144 A JP 2010161144A JP 2011037841 A5 JP2011037841 A5 JP 2011037841A5
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下記一般式［Ｉ］で表される化合物又はその医薬上許容される塩、或いはその溶媒和物：
Figure 2011037841
[式中、
部分構造式：
Figure 2011037841
は、下記式：
Figure 2011037841
で表される基のいずれかであり；
Ｒ１は、
（１）水素原子、
（２）Ｃ１−６アルキル基、
（３）Ｃ６−１４アリール基、
（４）Ｃ３−８シクロアルキル基、
（５）Ｃ６−１４アリール−Ｃ１−６アルキル基、又は、
（６）Ｃ３−８シクロアルキル−Ｃ１−６アルキル基であり；
Ｒ２は、
（１）水素原子、
（２）Ｃ１−１０アルキル基、
（３）下記グループＢから選ばれる同一又は異なった１乃至５個の置換基で置換されてもよいＣ６−１４アリール基、
（４）下記グループＢから選ばれる同一又は異なった１乃至５個の置換基で置換されてもよいＣ３−８シクロアルキル基、
（５）下記グループＢから選ばれる同一又は異なった１乃至５個の置換基で置換されてもよいＣ３−８シクロアルケニル基、
（６）下記グループＢから選ばれる同一又は異なった１乃至５個の置換基で置換されてもよいヘテロアリール基（ここで、該ヘテロアリールは、炭素原子の他に、窒素原子、酸素原子、及び、硫黄原子から選ばれる１乃至６個のヘテロ原子を有する）、
（７）Ｃ６−１４アリール−Ｃ１−６アルキル基（該Ｃ６−１４アリールは、下記グループＢから選ばれる同一又は異なった１乃至５個の置換基で置換されてもよい）、又は、
（８）Ｃ３−８シクロアルキル−Ｃ１−６アルキル基（該Ｃ３−８シクロアルキルは、下記グループＢから選ばれる同一又は異なった１乃至５個の置換基で置換されてもよい）であり；
Ｒ３は、
（１）水素原子、
（２）ハロゲン原子、
（３）Ｃ１−６アルキル基、
（４）Ｃ６−１４アリール基、
（５）Ｃ３−８シクロアルキル基、又は、
（６）Ｃ６−１４アリール−Ｃ１−６アルキル基であり；
Ｒ４及びＲ５は、それぞれ独立して、
（１）水素原子、又は、
（２）Ｃ１−６アルキル基である。
グループＢ：
（ａ）ハロゲン原子、
（ｂ）Ｃ１−６アルキル基、
（ｃ）Ｃ３−８シクロアルキル基、
（ｄ）シアノ基、及び
（ｅ）ハロ−Ｃ１−６アルキル基。]。 A compound represented by the following general formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof:
Figure 2011037841
[Where
Partial structural formula:
Figure 2011037841
Is the following formula:
Figure 2011037841
Any of the groups represented by
R 1 is
(1) a hydrogen atom,
(2) a C 1-6 alkyl group,
(3) a C 6-14 aryl group,
(4) a C 3-8 cycloalkyl group,
(5) a C 6-14 aryl-C 1-6 alkyl group, or
(6) is a C 3-8 cycloalkyl-C 1-6 alkyl group;
R 2 is
(1) a hydrogen atom,
(2) a C 1-10 alkyl group,
(3) a C 6-14 aryl group which may be substituted with the same or different 1 to 5 substituents selected from the following group B;
(4) a C 3-8 cycloalkyl group that may be substituted with 1 to 5 identical or different substituents selected from group B below,
(5) a C 3-8 cycloalkenyl group which may be substituted with the same or different 1 to 5 substituents selected from the following group B;
(6) A heteroaryl group which may be substituted with the same or different 1 to 5 substituents selected from the following group B (wherein the heteroaryl is a nitrogen atom, an oxygen atom, And 1 to 6 heteroatoms selected from sulfur atoms)
(7) a C 6-14 aryl-C 1-6 alkyl group (the C 6-14 aryl may be substituted with the same or different 1 to 5 substituents selected from group B below), or ,
(8) C 3-8 cycloalkyl-C 1-6 alkyl group (the C 3-8 cycloalkyl may be substituted with the same or different 1 to 5 substituents selected from group B below) Is;
R 3 is
(1) a hydrogen atom,
(2) a halogen atom,
(3) a C 1-6 alkyl group,
(4) a C 6-14 aryl group,
(5) a C 3-8 cycloalkyl group, or
(6) a C 6-14 aryl-C 1-6 alkyl group;
R 4 and R 5 are each independently
(1) a hydrogen atom or
(2) A C 1-6 alkyl group.
Group B:
(A) a halogen atom,
(B) a C 1-6 alkyl group,
(C) a C 3-8 cycloalkyl group,
(D) a cyano group, and (e) a halo-C 1-6 alkyl group. ]. 部分構造式：
Figure 2011037841
が、下記式
Figure 2011037841
で表される基である、請求項１記載の化合物又はその医薬上許容される塩、或いはその溶媒和物。 Partial structural formula:
Figure 2011037841
Is the following formula
Figure 2011037841
The compound of Claim 1 which is group represented by these, its pharmaceutically acceptable salt, or its solvate. 部分構造式：
Figure 2011037841
が、下記式
Figure 2011037841
で表される基である、請求項１記載の化合物又はその医薬上許容される塩、或いはその溶媒和物。 Partial structural formula:
Figure 2011037841
Is the following formula
Figure 2011037841
The compound of Claim 1 which is group represented by these, its pharmaceutically acceptable salt, or its solvate. 部分構造式：
Figure 2011037841
が、下記式
Figure 2011037841
で表される基である、請求項１記載の化合物又はその医薬上許容される塩、或いはその溶媒和物。 Partial structural formula:
Figure 2011037841
Is the following formula
Figure 2011037841
The compound of Claim 1 which is group represented by these, its pharmaceutically acceptable salt, or its solvate. 部分構造式：
Figure 2011037841
が、下記式
Figure 2011037841
で表される基である、請求項１記載の化合物又はその医薬上許容される塩、或いはその溶媒和物。 Partial structural formula:
Figure 2011037841
Is the following formula
Figure 2011037841
The compound of Claim 1 which is group represented by these, its pharmaceutically acceptable salt, or its solvate. Ｒ４及びＲ５がともに水素原子である、請求項１乃至５のいずれか１項に記載の化合物又はその医薬上許容される塩、或いはその溶媒和物。 The compound according to any one of claims 1 to 5, wherein R 4 and R 5 are both hydrogen atoms, or a pharmaceutically acceptable salt thereof, or a solvate thereof. Ｒ３が水素原子である、請求項１乃至５のいずれか１項に記載の化合物又はその医薬上許容される塩、或いはその溶媒和物。 The compound according to any one of claims 1 to 5, wherein R 3 is a hydrogen atom, or a pharmaceutically acceptable salt thereof, or a solvate thereof. Ｒ１が水素原子である、請求項１乃至５のいずれか１項に記載の化合物又はその医薬上許容される塩、或いはその溶媒和物。 The compound according to any one of claims 1 to 5, or a pharmaceutically acceptable salt thereof, or a solvate thereof, wherein R 1 is a hydrogen atom. Ｒ２が
（１）Ｃ１−１０アルキル基、
（２）前記グループＢから選ばれる同一又は異なった１乃至５個の置換基で置換されてもよいＣ６−１４アリール基、
（３）Ｃ６−１４アリール−Ｃ１−６アルキル基（該Ｃ６−１４アリールは、前記グループＢから選ばれる同一又は異なった１乃至５個の置換基で置換されてもよい）、又は、
（４）Ｃ３−８シクロアルキル−Ｃ１−６アルキル基（該Ｃ３−８シクロアルキルは、前記グループＢから選ばれる同一又は異なった１乃至５個の置換基で置換されてもよい）
である、請求項１乃至５のいずれか１項に記載の化合物又はその医薬上許容される塩、或いはその溶媒和物。 R 2 is (1) a C 1-10 alkyl group,
(2) a C 6-14 aryl group which may be substituted with 1 to 5 substituents which are the same or different from the group B;
(3) a C 6-14 aryl-C 1-6 alkyl group (the C 6-14 aryl may be substituted with the same or different 1 to 5 substituents selected from the group B), or ,
(4) C 3-8 cycloalkyl-C 1-6 alkyl group (the C 3-8 cycloalkyl may be substituted with the same or different 1 to 5 substituents selected from Group B)
The compound according to any one of claims 1 to 5, or a pharmaceutically acceptable salt thereof, or a solvate thereof. Ｒ４及びＲ５がともに水素原子である、請求項２に記載の化合物又はその医薬上許容される塩、或いはその溶媒和物。 The compound according to claim 2, wherein R 4 and R 5 are both hydrogen atoms, or a pharmaceutically acceptable salt thereof, or a solvate thereof. Ｒ３が水素原子である、請求項１０に記載の化合物又はその医薬上許容される塩、或いはその溶媒和物。 The compound according to claim 10, wherein R 3 is a hydrogen atom, or a pharmaceutically acceptable salt thereof, or a solvate thereof. Ｒ１が水素原子である、請求項１１に記載の化合物又はその医薬上許容される塩、或いはその溶媒和物。 The compound according to claim 11 or a pharmaceutically acceptable salt thereof, or a solvate thereof, wherein R 1 is a hydrogen atom. Ｒ２が
（１）Ｃ１−１０アルキル基、又は、
（２）Ｃ６−１４アリール−Ｃ１−６アルキル基（該Ｃ６−１４アリールは、前記グループＢから選ばれる同一又は異なった１乃至５個の置換基で置換されてもよい）
である、請求項１２に記載の化合物又はその医薬上許容される塩、或いはその溶媒和物。 R 2 is (1) a C 1-10 alkyl group, or
(2) C 6-14 aryl-C 1-6 alkyl group (the C 6-14 aryl may be substituted with the same or different 1 to 5 substituents selected from Group B)
The compound according to claim 12 or a pharmaceutically acceptable salt thereof, or a solvate thereof. 下記一般式［Ｉ−１］で表される化合物又はその医薬上許容される塩、或いはその溶媒和物：
Figure 2011037841
[式中、
部分構造式：
Figure 2011037841
は、下記式：
Figure 2011037841
で表される基のいずれかであり；
Ｒ１１は、
（１）水素原子、
（２）Ｃ１−６アルキル基、
（３）フェニル基、
（４）Ｃ３−８シクロアルキル基、
（５）フェニル−Ｃ１−６アルキル基、又は、
（６）Ｃ３−８シクロアルキル−Ｃ１−６アルキル基であり；
Ｒ２１は、
（１）水素原子、
（２）Ｃ１−１０アルキル基、
（３）下記グループＢから選ばれる同一又は異なった１乃至５個の置換基で置換されてもよいフェニル基、
（４）Ｃ３−８シクロアルキル基、
（５）Ｃ３−８シクロアルケニル基、
（６）下記グループＢから選ばれる同一又は異なった１乃至５個の置換基で置換されてもよいチエニル基、
（７）フェニル−Ｃ１−６アルキル基（該フェニルは、下記グループＢから選ばれる同一又は異なった１乃至５個の置換基で置換されてもよい）、又は、
（８）Ｃ３−８シクロアルキル−Ｃ１−６アルキル基であり；
Ｒ３１は、
（１）水素原子、
（２）ハロゲン原子、
（３）Ｃ１−６アルキル基、
（４）フェニル基、
（５）Ｃ３−８シクロアルキル基、又は、
（６）フェニル−Ｃ１−６アルキル基であり；
Ｒ４１及びＲ５１は、それぞれ独立して、
（１）水素原子、又は、
（２）Ｃ１−６アルキル基である。
グループＢ：
（ａ）ハロゲン原子、
（ｂ）Ｃ１−６アルキル基、
（ｃ）Ｃ３−８シクロアルキル基、
（ｄ）シアノ基、及び
（ｅ）ハロ−Ｃ１−６アルキル基。]。 A compound represented by the following general formula [I-1] or a pharmaceutically acceptable salt thereof, or a solvate thereof:
Figure 2011037841
[Where
Partial structural formula:
Figure 2011037841
Is the following formula:
Figure 2011037841
Any of the groups represented by
R 11 is
(1) a hydrogen atom,
(2) a C 1-6 alkyl group,
(3) phenyl group,
(4) a C 3-8 cycloalkyl group,
(5) a phenyl-C 1-6 alkyl group, or
(6) is a C 3-8 cycloalkyl-C 1-6 alkyl group;
R 21 is
(1) a hydrogen atom,
(2) a C 1-10 alkyl group,
(3) a phenyl group which may be substituted with the same or different 1 to 5 substituents selected from the following group B;
(4) a C 3-8 cycloalkyl group,
(5) a C 3-8 cycloalkenyl group,
(6) a thienyl group which may be substituted with 1 to 5 substituents which are the same or different from the following group B;
(7) a phenyl-C 1-6 alkyl group (the phenyl may be substituted with the same or different 1 to 5 substituents selected from group B below), or
(8) a C 3-8 cycloalkyl-C 1-6 alkyl group;
R 31 is
(1) a hydrogen atom,
(2) a halogen atom,
(3) a C 1-6 alkyl group,
(4) a phenyl group,
(5) a C 3-8 cycloalkyl group, or
(6) is a phenyl-C 1-6 alkyl group;
R 41 and R 51 are each independently
(1) a hydrogen atom or
(2) A C 1-6 alkyl group.
Group B:
(A) a halogen atom,
(B) a C 1-6 alkyl group,
(C) a C 3-8 cycloalkyl group,
(D) a cyano group, and (e) a halo-C 1-6 alkyl group. ]. 下記式：
Figure 2011037841
で表される化合物又はその医薬上許容される塩、或いはその溶媒和物。 Following formula:
Figure 2011037841
Or a pharmaceutically acceptable salt thereof, or a solvate thereof. 下記式：
Figure 2011037841
で表される化合物又はその医薬上許容される塩、或いはその溶媒和物。 Following formula:
Figure 2011037841
Or a pharmaceutically acceptable salt thereof, or a solvate thereof. 下記式：
Figure 2011037841
で表される化合物又はその医薬上許容される塩、或いはその溶媒和物。 Following formula:
Figure 2011037841
Or a pharmaceutically acceptable salt thereof, or a solvate thereof. 下記式：
Figure 2011037841
で表される化合物又はその医薬上許容される塩、或いはその溶媒和物。 Following formula:
Figure 2011037841
Or a pharmaceutically acceptable salt thereof, or a solvate thereof. 下記式：
Figure 2011037841
で表される化合物又はその医薬上許容される塩、或いはその溶媒和物。 Following formula:
Figure 2011037841
Or a pharmaceutically acceptable salt thereof, or a solvate thereof. 下記式：
Figure 2011037841
で表される化合物又はその医薬上許容される塩、或いはその溶媒和物。 Following formula:
Figure 2011037841
Or a pharmaceutically acceptable salt thereof, or a solvate thereof. 下記式：
Figure 2011037841
で表される化合物又はその医薬上許容される塩、或いはその溶媒和物。 Following formula:
Figure 2011037841
Or a pharmaceutically acceptable salt thereof, or a solvate thereof. 下記式：
Figure 2011037841
で表される化合物又はその医薬上許容される塩、或いはその溶媒和物。 Following formula:
Figure 2011037841
Or a pharmaceutically acceptable salt thereof, or a solvate thereof. 下記式：
Figure 2011037841
で表される化合物又はその医薬上許容される塩、或いはその溶媒和物。 Following formula:
Figure 2011037841
Or a pharmaceutically acceptable salt thereof, or a solvate thereof. 下記式：
Figure 2011037841
で表される化合物又はその医薬上許容される塩、或いはその溶媒和物。 Following formula:
Figure 2011037841
Or a pharmaceutically acceptable salt thereof, or a solvate thereof. 下記式：
Figure 2011037841
で表される化合物又はその医薬上許容される塩、或いはその溶媒和物。 Following formula:
Figure 2011037841
Or a pharmaceutically acceptable salt thereof, or a solvate thereof. 請求項１乃至２５のいずれか１項に記載の化合物又はその医薬上許容される塩、或いはその溶媒和物、及び医薬上許容される担体を含有する医薬組成物。   26. A pharmaceutical composition comprising the compound according to any one of claims 1 to 25 or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutically acceptable carrier. 請求項１乃至２５のいずれか１項に記載の化合物又はその医薬上許容される塩、或いはその溶媒和物を含有するプロリル水酸化酵素阻害剤。   A prolyl hydroxylase inhibitor comprising the compound according to any one of claims 1 to 25 or a pharmaceutically acceptable salt thereof, or a solvate thereof. 請求項１乃至２５のいずれか１項に記載の化合物又はその医薬上許容される塩、或いはその溶媒和物を含有するエリスロポエチン産生誘導剤。   An erythropoietin production inducer comprising the compound according to any one of claims 1 to 25 or a pharmaceutically acceptable salt thereof, or a solvate thereof. 請求項１乃至２５のいずれか１項に記載の化合物又はその医薬上許容される塩、或いはその溶媒和物を含有する貧血治療剤。   An anemia therapeutic agent comprising the compound according to any one of claims 1 to 25 or a pharmaceutically acceptable salt thereof, or a solvate thereof. 請求項１乃至２５のいずれか１項に記載の化合物又はその医薬上許容される塩、或いはその溶媒和物を含有する腎性貧血治療剤。   A therapeutic agent for renal anemia comprising the compound according to any one of claims 1 to 25 or a pharmaceutically acceptable salt thereof, or a solvate thereof. プロリル水酸化酵素阻害剤を製造するための、請求項１乃至２５のいずれか１項に記載の化合物又はその医薬上許容される塩、或いはその溶媒和物の使用。   Use of the compound according to any one of claims 1 to 25 or a pharmaceutically acceptable salt thereof, or a solvate thereof, for producing a prolyl hydroxylase inhibitor. エリスロポエチン産生誘導剤を製造するための、請求項１乃至２５のいずれか１項に記載の化合物又はその医薬上許容される塩、或いはその溶媒和物の使用。   Use of the compound according to any one of claims 1 to 25 or a pharmaceutically acceptable salt thereof, or a solvate thereof, for producing an erythropoietin production inducer. 貧血治療剤を製造するための、請求項１乃至２５のいずれか１項に記載の化合物又はその医薬上許容される塩、或いはその溶媒和物の使用。   Use of the compound according to any one of claims 1 to 25, or a pharmaceutically acceptable salt thereof, or a solvate thereof, for producing an anemia therapeutic agent. 腎性貧血治療剤を製造するための、請求項１乃至２５のいずれか１項に記載の化合物又はその医薬上許容される塩、或いはその溶媒和物の使用。   Use of the compound according to any one of claims 1 to 25 or a pharmaceutically acceptable salt thereof, or a solvate thereof, for producing a therapeutic agent for renal anemia. 請求項２６に記載の医薬組成物、及び当該医薬組成物を貧血及び腎性貧血より選ばれる疾患の治療又は予防の用途に使用することができる、或いは使用すべきであることを記載した当該医薬組成物に関する記載物を含む、商業パッケージ。   27. The pharmaceutical composition according to claim 26, and the said pharmaceutical composition, which can be used for the treatment or prevention of a disease selected from anemia and renal anemia, or should be used A commercial package containing a description of the composition. 請求項２６に記載の医薬組成物、及び当該医薬組成物を貧血及び腎性貧血より選ばれる疾患の治療又は予防の用途に使用することができる、或いは使用すべきであることを記載した当該医薬組成物に関する記載物を含む、キット。   27. The pharmaceutical composition according to claim 26, and the said pharmaceutical composition, which can be used for the treatment or prevention of a disease selected from anemia and renal anemia, or should be used A kit comprising a description relating to the composition.
JP2010161144A 2009-07-17 2010-07-16 Triazolopyridine compounds and their action as prolyl hydroxylase inhibitors and erythropoietin production inducers Active JP5021797B2 (en)

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